Abstract
Micromolar concentrations of methylmercury and several organic mercury fungicides were found to block binding of [3H]acetylcholine (ACh) to the ACh-receptor of the electric organ of the electric ray, Torpedo ocellata. The same compounds had little or no effect on the catalytic activity of ACh-esterase of the same tissue. [14C]Methyl-mercury bound to the purified ACh-receptor with high affinity (Kd= 7μM) and there were 6.5 ± 0.5 binding sites for each ACh-binding site. Binding of methylmercury was highly cooperative with a Hill coefficient of 2.6. This binding was irreversible by redialysis in methylmercury — free medium, however, the bound [14C]methylmercury was easily displaced from the receptor protein with μM concentrations of BAL or penicillamine. Methylmercury also blocked binding of [3H] nicotine and [3H]pilocarpine to the nicotinic and muscarinic ACh-receptors of the rat brain, respectively. The data suggest that the ACh-receptor may be a target for methylmercury and other organic mercury compounds.
This research was supported in part by National Science Foundation grant BMS 75–06760 and National Institutes of Health grant AI 12543 and NS 11280.
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Eldefrawi, M.E., Mansour, N.A., Eldefrawi, A.T. (1977). Interactions of Acetylcholine Receptors with Organic Mercury Compounds. In: Miller, M.W., Shamoo, A.E. (eds) Membrane Toxicity. Advances in Experimental Medicine and Biology, vol 84. Springer, Boston, MA. https://doi.org/10.1007/978-1-4684-3279-4_20
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